TWI804571B - 包含glp-1促效劑及n-(8-(2-羥苯甲醯基)胺基)辛酸之鹽的固體組成物 - Google Patents
包含glp-1促效劑及n-(8-(2-羥苯甲醯基)胺基)辛酸之鹽的固體組成物 Download PDFInfo
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- TWI804571B TWI804571B TW108103994A TW108103994A TWI804571B TW I804571 B TWI804571 B TW I804571B TW 108103994 A TW108103994 A TW 108103994A TW 108103994 A TW108103994 A TW 108103994A TW I804571 B TWI804571 B TW I804571B
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- A61K9/2013—Organic compounds, e.g. phospholipids, fats
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- A—HUMAN NECESSITIES
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- A61K38/17—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
- A61K38/22—Hormones
- A61K38/26—Glucagons
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- A—HUMAN NECESSITIES
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- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
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- A—HUMAN NECESSITIES
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- A61P3/00—Drugs for disorders of the metabolism
- A61P3/04—Anorexiants; Antiobesity agents
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- A—HUMAN NECESSITIES
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- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
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- C07K14/435—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
- C07K14/575—Hormones
- C07K14/605—Glucagons
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RS56998B1 (sr) | 2010-12-16 | 2018-05-31 | Novo Nordisk As | Čvrste kompozicije koje sadrže agonist glp-1 i so n-(8-(2-hidroksibenzoil)amino)kaprilne kiseline |
WO2012140117A1 (en) | 2011-04-12 | 2012-10-18 | Novo Nordisk A/S | Double-acylated glp-1 derivatives |
WO2013139694A1 (en) | 2012-03-22 | 2013-09-26 | Novo Nordisk A/S | Compositions of glp-1 peptides and preparation thereof |
KR102647171B1 (ko) | 2018-02-02 | 2024-03-15 | 노보 노르디스크 에이/에스 | Glp-1 작용제 및 n-(8-(2-하이드록시벤조일)아미노)카프릴산의 염을 포함하는 고형 조성물 |
TWI829687B (zh) | 2018-05-07 | 2024-01-21 | 丹麥商諾佛 儂迪克股份有限公司 | 包含glp-1促效劑與n-(8-(2-羥基苯甲醯基)胺基)辛酸之鹽的固體組成物 |
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CA3184717A1 (en) | 2020-07-22 | 2022-01-27 | Patrick J. KNERR | Co-agonists at glp-1 and gip receptors suitable for oral delivery |
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WO2022235991A1 (en) | 2021-05-07 | 2022-11-10 | Eli Lilly And Company | Erodible tablet |
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US20230053812A1 (en) * | 2021-07-27 | 2023-02-23 | Aurobindo Pharma Ltd | Stable peptide formulations for oral use |
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WO2023065231A1 (en) * | 2021-10-21 | 2023-04-27 | Guangzhou Dazhou Biomedicine Ltd. | Oral delivery of therapeutic agents |
CN118234742A (zh) * | 2021-12-01 | 2024-06-21 | 江苏恒瑞医药股份有限公司 | Glp-1和gip受体双重激动剂的药物组合物及其用途 |
IL312382A (en) * | 2021-12-11 | 2024-06-01 | Imagine Pharma Llc | COMPOUNDS AND METHODS OF ORAL ADMINISTRATION |
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EP4337244A1 (en) * | 2022-03-25 | 2024-03-20 | Beijing QL Biopharmaceutical Co., Ltd. | Pharmaceutical compositions of polypeptide conjugates and methods of uses thereof |
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CN114984191B (zh) * | 2022-07-04 | 2022-10-25 | 北京惠之衡生物科技有限公司 | 一种多肽类药物口服递送组合物 |
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Citations (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
JP2014503526A (ja) * | 2010-12-16 | 2014-02-13 | ノヴォ ノルディスク アー/エス | Glp−1アゴニストとn−(8−(2−ヒドロキシベンゾイル)アミノ)カプリル酸の塩とを含む固形組成物 |
Family Cites Families (196)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US278923A (en) * | 1883-06-05 | Newspapee weappee | ||
PH24180A (en) | 1986-03-12 | 1990-03-22 | Glaxo Group Ltd | Macrolide compounds,pharmaceutical composition containing said compound and method of use thereof |
CA2073856C (en) | 1990-01-24 | 2002-12-03 | Douglas I. Buckley | Glp-1 analogs useful for diabetes treatment |
US5545618A (en) | 1990-01-24 | 1996-08-13 | Buckley; Douglas I. | GLP-1 analogs useful for diabetes treatment |
DK39892D0 (da) | 1992-03-25 | 1992-03-25 | Bernard Thorens | Peptid |
HUT73494A (en) | 1993-03-29 | 1996-08-28 | Univ Cincinnati | Analogs of peptide yy and uses thereof |
US5705483A (en) | 1993-12-09 | 1998-01-06 | Eli Lilly And Company | Glucagon-like insulinotropic peptides, compositions and methods |
US5968899A (en) | 1994-06-03 | 1999-10-19 | Tsumura & Co. | Medicinal compositions of peptides with EACA or tranexamic acid for enhanced mucosal absorption |
US5512549A (en) | 1994-10-18 | 1996-04-30 | Eli Lilly And Company | Glucagon-like insulinotropic peptide analogs, compositions, and methods of use |
US5574010A (en) | 1994-11-14 | 1996-11-12 | The Regents Of The University Of California | Treatment of pancreatic tumors with peptide YY and analogs thereof |
US5869602A (en) | 1995-03-17 | 1999-02-09 | Novo Nordisk A/S | Peptide derivatives |
US5866536A (en) | 1995-03-31 | 1999-02-02 | Emisphere Technologies, Inc. | Compounds and compositions for delivering active agents |
US5650386A (en) | 1995-03-31 | 1997-07-22 | Emisphere Technologies, Inc. | Compositions for oral delivery of active agents |
SE9600070D0 (sv) | 1996-01-08 | 1996-01-08 | Astra Ab | New oral pharmaceutical dosage forms |
US6458924B2 (en) | 1996-08-30 | 2002-10-01 | Novo Nordisk A/S | Derivatives of GLP-1 analogs |
JP3149958B2 (ja) | 1996-08-30 | 2001-03-26 | ノボ ノルディスク アクティーゼルスカブ | Glp―1誘導体 |
US6268343B1 (en) | 1996-08-30 | 2001-07-31 | Novo Nordisk A/S | Derivatives of GLP-1 analogs |
US7235627B2 (en) | 1996-08-30 | 2007-06-26 | Novo Nordisk A/S | Derivatives of GLP-1 analogs |
JP2001504105A (ja) | 1996-11-12 | 2001-03-27 | ノボ ノルディスク アクティーゼルスカブ | Glp―1ペプチドの利用 |
AU1159897A (en) | 1996-11-13 | 1998-06-03 | University Of Cincinnati, The | Analogs of peptide yy and uses thereof |
US5773647A (en) | 1997-02-07 | 1998-06-30 | Emisphere Technologies, Inc. | Compounds and compositions for delivering active agents |
EP0908515A3 (en) | 1997-09-16 | 2000-04-26 | Smithkline Beecham Plc | Pancreatic polypeptide |
JP2002512175A (ja) | 1998-02-27 | 2002-04-23 | ノボ ノルディスク アクティーゼルスカブ | Glp−1類似体の誘導体類 |
WO1999043708A1 (en) | 1998-02-27 | 1999-09-02 | Novo Nordisk A/S | Glp-1 derivatives of glp-1 and exendin with protracted profile of action |
AU2610599A (en) | 1998-02-27 | 1999-09-15 | Novo Nordisk A/S | N-terminally truncated glp-1 derivatives |
AU2610899A (en) | 1998-02-27 | 1999-09-15 | Novo Nordisk A/S | N-terminally modified glp-1 derivatives |
ATE265224T1 (de) | 1998-02-27 | 2004-05-15 | Novo Nordisk As | Glp-1 derivate mit einem helix-gehalt über 25 , die partiell strukturierte mizellenartige aggregate bilden |
US6046167A (en) | 1998-03-25 | 2000-04-04 | University Of Cincinnati | Peptide YY analogs |
AU4317899A (en) | 1998-06-08 | 1999-12-30 | Schering Corporation | Neuropeptide y5 receptor antagonists |
SE9802080D0 (sv) | 1998-06-11 | 1998-06-11 | Hellstroem | Pharmaceutical composition for the treatment of functional dyspepsia and/or irritable bowel syndrome and new use of substances therein |
DE69911975T2 (de) | 1998-07-31 | 2004-09-09 | Novo Nordisk A/S | In-vitro stimulation von beta zellen vermehrung |
MY155270A (en) | 1998-09-24 | 2015-09-30 | Lilly Co Eli | Use of glp-1 or analogs in treatment of stroke |
CZ295891B6 (cs) | 1998-12-07 | 2005-11-16 | Societe De Conseils De Recherches Et D'application | Analogy GLP-1, substituované na pozici 35, jejich použití a farmaceutické prostředky je obsahující |
EP1149066B1 (en) | 1999-02-05 | 2005-11-09 | Emisphere Technologies, Inc. | Method of preparing alkylated salicylamides |
WO2000048589A1 (en) | 1999-02-22 | 2000-08-24 | Emisphere Holdings, Inc. | Solid oral dosage form containing heparin or a heparinoid in combination with a carrier |
US7658938B2 (en) | 1999-02-22 | 2010-02-09 | Merrion Reasearch III Limited | Solid oral dosage form containing an enhancer |
AU2681300A (en) | 1999-02-22 | 2000-09-14 | Elan Corporation, Plc | Solid oral dosage form containing an enhancer |
BR0010705A (pt) | 1999-04-30 | 2002-02-05 | Amylin Pharmaceuticals Inc | Exendinas modificadas e agonistas da exendina |
EA003922B1 (ru) | 1999-05-17 | 2003-10-30 | Конджачем, Инк. | Продолжительно действующие инсулинотропные пептиды |
US7601691B2 (en) | 1999-05-17 | 2009-10-13 | Conjuchem Biotechnologies Inc. | Anti-obesity agents |
EP1076066A1 (en) | 1999-07-12 | 2001-02-14 | Zealand Pharmaceuticals A/S | Peptides for lowering blood glucose levels |
GB9923436D0 (en) | 1999-10-04 | 1999-12-08 | American Home Prod | Pharmaceutical compositions |
US6793934B1 (en) | 1999-12-08 | 2004-09-21 | Shire Laboratories, Inc. | Solid oral dosage form |
AU2001275231A1 (en) | 2000-06-02 | 2001-12-11 | Emisphere Technologies, Inc. | Method of preparing salicylamides |
US7049283B2 (en) | 2000-12-06 | 2006-05-23 | Novartis Ag | Pharmaceutical compositions for the oral delivery of pharmacologically active agents |
CA2716959A1 (en) | 2000-12-07 | 2002-06-13 | Eli Lilly And Company | Glp-1 fusion proteins |
EP1351984A2 (en) | 2000-12-13 | 2003-10-15 | Eli Lilly And Company | Amidated glucagon-like peptide-1 |
AU2002230843B8 (en) | 2000-12-14 | 2007-05-17 | Amylin Pharmaceuticals, Llc | Peptide YY and peptide YY agonists for treatment of metabolic disorders |
US6589938B2 (en) | 2001-06-29 | 2003-07-08 | National University Of Singapore | Use of angiotensin I derivatives as an agent for the treatment and prevention of infarction-related cardiac injuries and disorders |
US20030068356A1 (en) | 2001-07-10 | 2003-04-10 | Pather S. Indiran | Sequential drug delivery systems |
CA2455963C (en) | 2001-07-31 | 2017-07-04 | The Government Of The United States Of America As Represented By The Secretary, Department Of Health And Human Services | Glp-1, exendin-4, peptide analogs and uses thereof |
ES2320979T3 (es) | 2001-09-24 | 2009-06-01 | Imperial Innovations Limited | Pyy-36 para la reduccion o prevencion de la obesidad. |
JP5196701B2 (ja) | 2001-11-29 | 2013-05-15 | エミスフィアー テクノロジーズ インコーポレイテッド | クロモリンナトリウムの経口投与用製剤 |
US8058233B2 (en) | 2002-01-10 | 2011-11-15 | Oregon Health And Science University | Modification of feeding behavior using PYY and GLP-1 |
JP2005526020A (ja) | 2002-02-01 | 2005-09-02 | ファイザー・プロダクツ・インク | アジスロマイシンの乾式造粒配合物 |
US20050148497A1 (en) | 2002-02-20 | 2005-07-07 | Khan Mohammed A. | Method for administering glp-1 molecules |
ES2327328T3 (es) | 2002-07-04 | 2009-10-28 | Zealand Pharma A/S | Glp-1 y procedimientos para el tratamiento de la diabetes. |
JP2004131398A (ja) | 2002-10-08 | 2004-04-30 | Taihei Chemical Industrial Co Ltd | 錠剤用滑沢剤 |
EP1583549A4 (en) | 2003-01-17 | 2006-10-04 | Sod Conseils Rech Applic | YY PEPTIDE ANALOGS |
US20050059605A1 (en) | 2003-01-31 | 2005-03-17 | Krishna Peri | Chemically modified metabolites of regulatory peptides and methods of producing and using same |
SI1605897T1 (sl) | 2003-03-19 | 2012-11-30 | Lilly Co Eli | Polietilen glikol povezane GLP spojine |
WO2004104018A2 (en) | 2003-05-14 | 2004-12-02 | Emisphere Technologies, Inc. | Compositions for delivering peptide yy and pyy agonists |
US7572581B2 (en) | 2003-06-30 | 2009-08-11 | Roche Molecular Systems, Inc. | 2′-terminator nucleotide-related methods and systems |
CN1809377B (zh) | 2003-07-11 | 2010-08-04 | 诺瓦提斯公司 | 包含微粉化形式的传送剂的口服给药药物组合物 |
EP1653996A2 (en) | 2003-08-08 | 2006-05-10 | Novo Nordisk Health Care AG | Use of galactose oxidase for selective chemical conjugation of protractor molecules to proteins of therapeutic interest |
CN100444898C (zh) | 2003-09-19 | 2008-12-24 | 诺沃挪第克公司 | 治疗肽的清蛋白结合型衍生物 |
WO2005028516A2 (en) | 2003-09-19 | 2005-03-31 | Novo Nordisk A/S | Albumin-binding derivatives of therapeutic peptides |
US20070203058A1 (en) | 2003-09-19 | 2007-08-30 | Novo Nordisk A/S | Novel Glp-1 Derivatives |
HUE038395T2 (hu) | 2003-11-20 | 2018-10-29 | Novo Nordisk As | Propilén-glikol tartalmú peptidkészítmények, amelyek elõállításra és injekciós eszközökben történõ alkalmazásra optimálisak |
DE602004026113D1 (de) | 2003-12-18 | 2010-04-29 | Novo Nordisk As | Glp-1-verbindungen |
RU2006120077A (ru) | 2003-12-18 | 2008-01-27 | Ново Нордиск А/С (DK) | Аналоги глюкагоноподобного пептида-1 (glp-1), связанные с альбуминоподобными агентами |
US20060286129A1 (en) | 2003-12-19 | 2006-12-21 | Emisphere Technologies, Inc. | Oral GLP-1 formulations |
AU2005211776B2 (en) | 2004-02-11 | 2012-02-02 | Amylin Pharmaceuticals, Llc | Pancreatic polypeptide family motifs and polypeptides comprising the same |
CN1961000B (zh) | 2004-02-11 | 2011-05-04 | 安米林药品公司 | 具有可选择特性的杂合多肽 |
CN100425282C (zh) | 2004-03-17 | 2008-10-15 | 7Tm制药联合股份有限公司 | 用于治疗性干预的y2/y4选择性受体激动剂 |
DK2060266T3 (da) | 2004-03-17 | 2011-11-14 | 7Tm Pharma As | Y4-selektiv receptoragonist PP2-36 til terapeutiske indgreb |
WO2005089789A2 (en) | 2004-03-17 | 2005-09-29 | 7Tm Pharma A/S | Y2 selective receptor agonists for therapeutic interventions |
US20080261871A1 (en) | 2004-03-17 | 2008-10-23 | 7Tm Pharma A/S | Y2/Y4 Selective Receptor Agonists for Therapeutic Interventions |
WO2005099672A1 (en) | 2004-04-13 | 2005-10-27 | Ranbaxy Laboratories Limited | A modified release pharmaceutical formulation comprising amoxicillin and clavulanate |
US8039018B2 (en) | 2004-05-06 | 2011-10-18 | Emisphere Technologies, Inc. | Solid dosage form of wetted heparin |
EA013518B1 (ru) | 2004-05-06 | 2010-06-30 | Эмисфире Текнолоджис, Инк. | Кристаллические полиморфные формы n-[8-(2-гидроксибензоил)амино]каприлата натрия |
CA2565188C (en) | 2004-05-14 | 2014-03-04 | Emisphere Technologies, Inc. | Compounds and compositions for delivering active agents |
GB0412181D0 (en) | 2004-06-01 | 2004-06-30 | Celltech R&D Ltd | Biological products |
WO2005121090A1 (en) | 2004-06-02 | 2005-12-22 | Abbott Laboratories | Substituted piperidines that have antiangiogenic activity |
CN101010339B (zh) | 2004-07-02 | 2011-11-09 | 布里斯托尔-迈尔斯斯奎布公司 | 人类胰高血糖素样肽-1调节剂及它们在治疗糖尿病及相关病况中的用途 |
TW200611704A (en) | 2004-07-02 | 2006-04-16 | Bristol Myers Squibb Co | Human glucagon-like-peptide-1 modulators and their use in the treatment of diabetes and related conditions |
BRPI0512988A (pt) | 2004-07-08 | 2008-04-22 | Novo Nordisk As | método para aumentar a meia-vida plasmática de uma molécula, composto, uso do mesmo, e, composição farmacêutica |
NZ552558A (en) | 2004-07-12 | 2009-11-27 | Emisphere Tech Inc | Compositions for delivering peptide YY and PYY agonists |
WO2006020207A2 (en) | 2004-07-19 | 2006-02-23 | University Of Cincinnati | Compounds for control of appetite |
US20060078622A1 (en) | 2004-08-13 | 2006-04-13 | Emisphere Technologies, Inc. | Pharmaceutical formulations containing microparticles or nanoparticles of a delivery agent |
WO2006049681A2 (en) | 2004-08-30 | 2006-05-11 | Bayer Pharmaceuticals Corporation | Selective neuropeptide y2 receptor agonists |
JP5107713B2 (ja) | 2004-10-07 | 2012-12-26 | ノヴォ ノルディスク アー/エス | 遅延性のエキセンディン−4化合物 |
EP1799710A2 (en) | 2004-10-07 | 2007-06-27 | Novo Nordisk A/S | Protracted glp-1 compounds |
US7410949B2 (en) | 2005-01-18 | 2008-08-12 | Hoffmann-La Roche Inc. | Neuropeptide-2 receptor (Y-2R) agonists and uses thereof |
US20080153779A1 (en) | 2005-02-01 | 2008-06-26 | Jun Liao | Gastric Retention and Controlled Release Delivery System |
EP1846446B1 (en) | 2005-02-02 | 2013-06-26 | Novo Nordisk A/S | Insulin derivatives |
EP1858546A4 (en) | 2005-03-04 | 2009-03-04 | Biorexis Pharmaceutical Corp | MODIFIED TRANSFERRINFUSION PROTEINS |
GB0504857D0 (en) | 2005-03-09 | 2005-04-13 | Imp College Innovations Ltd | Novel compounds and their effects on feeding behaviour |
WO2006097535A2 (en) | 2005-03-18 | 2006-09-21 | Novo Nordisk A/S | Peptide agonists of the glucagon family with secretin like activity |
EP1863521B1 (en) | 2005-03-18 | 2014-05-07 | Novo Nordisk A/S | Extended glp-1 compounds |
TWI362392B (en) | 2005-03-18 | 2012-04-21 | Novo Nordisk As | Acylated glp-1 compounds |
EP1863537A2 (en) | 2005-03-18 | 2007-12-12 | Novo Nordisk A/S | Dimeric peptide agonists of the glp-1 receptor |
WO2006103661A2 (en) | 2005-03-28 | 2006-10-05 | Dexcel Pharma Technologies Ltd. | Controlled absorption of statins in the intestine |
AU2006249869A1 (en) | 2005-05-26 | 2006-11-30 | Bristol-Myers Squibb Company | N-terminally modified GLP-1 receptor modulators |
EP1907008A2 (en) | 2005-07-11 | 2008-04-09 | Nastech Pharmaceutical Company Inc. | Formulations for enhanced mucosal delivery of pyy |
US8975227B2 (en) | 2005-07-15 | 2015-03-10 | Emisphere Technologies, Inc. | Intraoral dosage forms of glucagon |
CA2616583A1 (en) | 2005-07-18 | 2007-01-25 | Novo-Nordisk A/S | Peptides for use in the treatment of obesity |
CA2619426C (en) | 2005-08-19 | 2016-06-21 | Amylin Pharmaceuticals, Inc. | Exendin for treating diabetes and reducing body weight |
US20070049557A1 (en) | 2005-08-24 | 2007-03-01 | Hashim Ahmed | Solid pharmaceutical dosage forms comprising bisphosphonates and modified amino acid carriers |
US8022035B2 (en) | 2005-09-21 | 2011-09-20 | 7Tm Pharma A/S | Y4 selective receptor agonists for therapeutic interventions |
EP1934245B1 (en) | 2005-09-21 | 2011-07-13 | 7TM Pharma A/S | Y2 selective receptor agonists for therapeutic interventions |
WO2007061434A2 (en) | 2005-11-10 | 2007-05-31 | Nastech Pharmaceutical Company Inc. | A pharmaceutical formulation of glp-1 and its use for treating a metabolic syndrome |
KR20140053419A (ko) | 2005-11-17 | 2014-05-07 | 노파르티스 아게 | 약제학적 조성물 |
WO2007065808A2 (en) | 2005-12-07 | 2007-06-14 | F. Hoffmann-La Roche Ag | Neuropeptide-2 receptor-agonists |
EP1959987A2 (en) | 2005-12-08 | 2008-08-27 | Nastech Pharmaceutical Company Inc. | Mucosal delivery of stabilized formulations of exendin |
WO2007068718A1 (en) | 2005-12-14 | 2007-06-21 | Novo Nordisk A/S | Polypeptide protracting tags |
US20070197445A1 (en) | 2006-01-18 | 2007-08-23 | University Of Cincinnati | Compounds for control of appetite |
CN101432025B (zh) | 2006-03-21 | 2012-04-04 | 安米林药品公司 | 肽-肽酶抑制剂结合物及其使用方法 |
EP2007397B1 (en) | 2006-04-07 | 2013-07-24 | Merrion Research III Limited | Solid oral dosage form containing an enhancer |
US8927015B2 (en) | 2006-04-12 | 2015-01-06 | Emisphere Technologies, Inc. | Formulations for delivering insulin |
MX2008014061A (es) | 2006-05-09 | 2008-11-14 | Novo Nordisk As | Derivado de insulina. |
WO2007146234A2 (en) | 2006-06-09 | 2007-12-21 | Merrion Research Ii Limited | Solid oral dosage form containing an enhancer |
US9364502B2 (en) | 2006-06-28 | 2016-06-14 | Emisphere Technologies, Inc. | Gallium nitrate formulations |
GB0613196D0 (en) | 2006-07-03 | 2006-08-09 | Imp Innovations Ltd | Novel compounds and their effects on feeding behaviour |
ES2296529B1 (es) | 2006-08-07 | 2009-04-01 | Laboratorios Farmaceuticos Rovi, S.A. | Composicion farmaceutica con promotores de absorcion. |
EP2057189B1 (en) | 2006-08-25 | 2013-03-06 | Novo Nordisk A/S | Acylated exendin-4 compounds |
US7544833B2 (en) | 2006-09-07 | 2009-06-09 | Hoffmann-La Roche Inc. | Methods for producing N-(8-[2-hydroxybenzoyl]-amino) caprylic acid |
PE20080840A1 (es) | 2006-09-13 | 2008-08-27 | Smithkline Beecham Corp | Metodos para administrar agentes hipoglucemiantes de larga duracion |
AR062925A1 (es) | 2006-09-22 | 2008-12-17 | Novartis Ag | Metodo para fabricar tabletas que contienen agentes farmacologicamente activos |
GB0621973D0 (en) | 2006-11-03 | 2006-12-13 | Philogen Spa | Binding molecules and uses thereof |
WO2008070547A1 (en) | 2006-12-01 | 2008-06-12 | Emisphere Technologies Inc. | Improved acyclovir formulations |
US20090099074A1 (en) | 2007-01-10 | 2009-04-16 | Conjuchem Biotechnologies Inc. | Modulating food intake |
JP2010516652A (ja) | 2007-01-18 | 2010-05-20 | ノボ・ノルデイスク・エー/エス | 肥満の治療に使用される新規ペプチド |
EP2101822A2 (en) | 2007-01-18 | 2009-09-23 | Novo Nordisk A/S | Use of peptides in combination with surgical intervention for the treatment of obesity |
DE602008006700D1 (es) | 2007-03-02 | 2011-06-16 | Novartis Ag | |
GB0708226D0 (en) | 2007-04-27 | 2007-06-06 | 7Tm Pharma As | Y-receptor agonists |
JP2010530962A (ja) | 2007-06-12 | 2010-09-16 | グラクソスミスクライン・リミテッド・ライアビリティ・カンパニー | 血漿においてタンパク質を検出する方法 |
CN101970475A (zh) | 2007-07-09 | 2011-02-09 | 帝国改革有限公司 | 人类胰多肽(hpp)类似物及其对摄食行为的作用 |
CN101842101A (zh) | 2007-08-29 | 2010-09-22 | 加利福尼亚大学董事会 | 水杨酰苯胺修饰的肽用作口服治疗剂 |
US8895694B2 (en) | 2007-09-05 | 2014-11-25 | Novo Nordisk A/S | Glucagon-Like Peptide-1 derivatives and their pharmaceutical use |
EP2190873B1 (en) | 2007-09-05 | 2015-07-22 | Novo Nordisk A/S | Truncated glp-1 derivatives and their therapeutical use |
US20100261637A1 (en) | 2007-09-05 | 2010-10-14 | Novo Nordisk A/S | Peptides derivatized with a-b-c-d- and their therapeutical use |
CA2698968A1 (en) | 2007-09-11 | 2009-03-19 | Mondobiotech Laboratories Ag | Use of a peptide as a therapeutic agent |
US8598314B2 (en) | 2007-09-27 | 2013-12-03 | Amylin Pharmaceuticals, Llc | Peptide-peptidase-inhibitor conjugates and methods of making and using same |
WO2009050738A2 (en) | 2007-10-16 | 2009-04-23 | Biocon Limited | An orally administerable solid pharmaceutical composition and a process thereof |
PL2215047T3 (pl) | 2007-11-02 | 2014-05-30 | Emisphere Tech Inc | Sposób leczenia niedoborów witaminy b12 |
US20090124639A1 (en) | 2007-11-06 | 2009-05-14 | Emisphere Technologies Inc. | valacyclovir formulations |
US20100317057A1 (en) | 2007-12-28 | 2010-12-16 | Novo Nordisk A/S | Semi-recombinant preparation of glp-1 analogues |
BRPI0912615A2 (pt) | 2008-05-16 | 2016-01-26 | Novo Nordisk As | agonistas de receptor y2 e/ou y4 de longa ação |
AU2009283821B2 (en) | 2008-08-18 | 2014-05-29 | Entera Bio Ltd. | Methods and compositions for oral administration of proteins |
CN102149411A (zh) | 2008-09-12 | 2011-08-10 | 诺沃—诺迪斯克有限公司 | 酰化肽或蛋白的方法 |
US8299023B2 (en) | 2008-09-17 | 2012-10-30 | Hoffmann-La Roche Inc. | Neuropeptide-2 receptor (Y-2R) agonists |
GB0817067D0 (en) | 2008-09-18 | 2008-10-22 | 7Tm Pharma As | Intestinal treatment |
EP2271219B1 (de) | 2008-10-15 | 2011-11-23 | Bayer CropScience AG | Verwendung von dithiin-tetracarboximiden zum bekämpfen phytopathogener pilze |
MX2011004427A (es) | 2008-11-05 | 2011-05-31 | Hoffmann La Roche | Agonistas del receptor de neuropeptido-2 (y-2r) y usos de los mismos. |
CN101463081B (zh) | 2009-01-12 | 2012-07-04 | 华东师范大学 | 一种glp-1衍生物 |
AU2010212823B2 (en) | 2009-02-13 | 2016-01-28 | Boehringer Ingelheim International Gmbh | Antidiabetic medications comprising a DPP-4 inhibitor (linagliptin) optionally in combination with other antidiabetics |
BRPI1008039A2 (pt) | 2009-02-20 | 2016-10-04 | Ipsen Pharma Sas | composto, mistura, composição farmacêutica, e, uso de um coposto, de uma mistura ou de uma composição farmacêutica |
AR077956A1 (es) | 2009-09-14 | 2011-10-05 | Bayer Cropscience Ag | Combinaciones de compuestos activos |
JP2013505221A (ja) | 2009-09-18 | 2013-02-14 | ノヴォ ノルディスク アー/エス | 長時間作用性y2受容体アゴニスト |
JP2013507414A (ja) | 2009-10-13 | 2013-03-04 | エフ.ホフマン−ラ ロシュ アーゲー | 神経ペプチド−2受容体(y−2r)アゴニスト |
US20130096055A1 (en) | 2009-11-13 | 2013-04-18 | Novo Nordisk A/S | Long-acting y2 receptor agonists |
CN102791731B (zh) | 2009-12-16 | 2016-04-20 | 诺沃—诺迪斯克有限公司 | Glp-1类似物和衍生物 |
AU2010339907A1 (en) | 2009-12-16 | 2012-07-05 | Nod Pharmaceuticals, Inc. | Compositions and methods for oral drug delivery |
US20110182985A1 (en) | 2010-01-28 | 2011-07-28 | Coughlan David C | Solid Pharmaceutical Composition with Enhancers and Methods of Preparing thereof |
WO2011109787A1 (en) | 2010-03-05 | 2011-09-09 | Conjuchem, Llc | Methods of administering insulinotropic peptides |
GB2478849A (en) | 2010-03-16 | 2011-09-21 | Chiasma Inc | Improved pharmecutical compositions and methods of delivery |
EP2560675A1 (en) | 2010-04-20 | 2013-02-27 | Novo Nordisk A/S | Long-acting gastrin derivatives |
CA2793715A1 (en) | 2010-04-30 | 2011-11-03 | Sanwa Kagaku Kenkyusho Co., Ltd. | Peptide for improving in vivo stability of physiologically active substance or the like and physiologically active substance with improved in vivo stability |
WO2011138421A1 (en) | 2010-05-05 | 2011-11-10 | Boehringer Ingelheim International Gmbh | Combination therapy |
DE202010015867U1 (de) | 2010-11-25 | 2011-05-05 | Buchhalter, Thomas | Elektromechanische Halterung zur Aufnahme von Navigations- und Kommunikationsgeräte im KFZ |
GB201101459D0 (en) | 2011-01-27 | 2011-03-16 | Imp Innovations Ltd | Novel compounds and thier effects on fedding behaviour |
WO2012140117A1 (en) | 2011-04-12 | 2012-10-18 | Novo Nordisk A/S | Double-acylated glp-1 derivatives |
WO2013009545A1 (en) | 2011-07-08 | 2013-01-17 | Amylin Pharmaceuticals, Inc. | Engineered polypeptides having enhanced duration of action with reduced immunogenicity |
DE102012102301B4 (de) | 2012-03-19 | 2021-06-17 | OSRAM Opto Semiconductors Gesellschaft mit beschränkter Haftung | Optoelektronischer Halbleiterchip und Scheinwerfer mit einem solchen Halbleiterchip |
CN104203221A (zh) * | 2012-03-22 | 2014-12-10 | 诺和诺德A/S(股份有限公司) | 包含递送剂的组合物及其制备 |
WO2013139694A1 (en) | 2012-03-22 | 2013-09-26 | Novo Nordisk A/S | Compositions of glp-1 peptides and preparation thereof |
HUE042757T2 (hu) | 2012-03-22 | 2019-07-29 | Novo Nordisk As | Szállító szert tartalmazó készítmények és elõállításuk |
WO2013178490A1 (en) | 2012-05-29 | 2013-12-05 | Novo Nordisk A/S | Pancreatic polypeptide compounds and use |
WO2013189988A1 (en) | 2012-06-20 | 2013-12-27 | Novo Nordisk A/S | Tablet formulation comprising a peptide and a delivery agent |
CA2877056A1 (en) | 2012-07-01 | 2014-01-09 | Novo Nordisk A/S | Use of long-acting glp-1 peptides |
EA201591839A1 (ru) | 2013-05-02 | 2016-05-31 | Глаксосмитклайн Интеллекчуал Проперти Дивелопмент Лимитед | Терапевтические пептиды |
US20160067184A1 (en) | 2013-05-02 | 2016-03-10 | Novo Nordisk A/S | Oral Dosing of GLP-1 Compounds |
CN105722526B (zh) | 2013-11-15 | 2020-12-08 | 诺和诺德股份有限公司 | 选择性pyy化合物及其用途 |
US10583172B2 (en) | 2013-11-15 | 2020-03-10 | Novo Nordisk A/S | HPYY(1-36) having a beta-homoarginine substitution at position 35 |
JP6768515B2 (ja) | 2014-04-07 | 2020-10-14 | ノヴォ ノルディスク アー/エス | 二重アシル化glp−1化合物 |
JOP20200119A1 (ar) | 2015-01-09 | 2017-06-16 | Lilly Co Eli | مركبات مساعد مشترك من gip وglp-1 |
US20180263915A1 (en) * | 2015-01-29 | 2018-09-20 | Novo Nordisk A/S | Pharmaceutical Composition for Oral GLP-1 Administration Comprising a Tablet Core and Immediate Release Coating |
CA2975578A1 (en) | 2015-02-09 | 2016-08-18 | Entera Bio Ltd. | Treatment of hypoparathyroidism |
KR102476550B1 (ko) | 2015-06-12 | 2022-12-13 | 노보 노르디스크 에이/에스 | 선택적인 pyy 화합물 및 그것의 사용 |
AU2016335287A1 (en) * | 2015-10-07 | 2018-04-12 | Cyprumed Gmbh | Pharmaceutical formulations for the oral delivery of peptide drugs |
TWI797133B (zh) | 2017-06-09 | 2023-04-01 | 丹麥商諾佛 儂迪克股份有限公司 | 用於經口投予的固體組成物 |
TWI762706B (zh) | 2017-08-24 | 2022-05-01 | 丹麥商諾佛 儂迪克股份有限公司 | Glp-1組成物及其用途 |
KR102647171B1 (ko) | 2018-02-02 | 2024-03-15 | 노보 노르디스크 에이/에스 | Glp-1 작용제 및 n-(8-(2-하이드록시벤조일)아미노)카프릴산의 염을 포함하는 고형 조성물 |
TWI829687B (zh) | 2018-05-07 | 2024-01-21 | 丹麥商諾佛 儂迪克股份有限公司 | 包含glp-1促效劑與n-(8-(2-羥基苯甲醯基)胺基)辛酸之鹽的固體組成物 |
WO2021023811A1 (en) * | 2019-08-07 | 2021-02-11 | Novo Nordisk A/S | Solid compositions comprising a glp-1 agonist, an sglt2 inhibitor and a salt of n-(8-(2-hydroxybenzoyl)amino)caprylic acid |
-
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Patent Citations (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
JP2014503526A (ja) * | 2010-12-16 | 2014-02-13 | ノヴォ ノルディスク アー/エス | Glp−1アゴニストとn−(8−(2−ヒドロキシベンゾイル)アミノ)カプリル酸の塩とを含む固形組成物 |
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